Adrenergic drugs- direct acting Catecholamines Flashcards
MoA of Adrenergic drugs?
Stimulate α & β adrenergic and dopamine receptors –> mimic the action of Epinephrine (E) & Norepinephrine (NE).
Subtypes of Adrenergic drugs
Catecholamines & non-catecholamines
MoA of Catecholamine drugs
direct-acting, indirect-acting & dual-acting.
Routes of Administraions of Cathecolamines
Intramuscullary (I.M.)–> rapid absorptin
others :
NOT orally used –> metabolized by digestive enzymes.
SL –> rapid absorption through mucus membranes.
S.C –> slow absorption
Metabolism of Catecholamines
–> Meablised in the liver (COMT and MAO)
also in the GI tract, lungs, kidneys, plasma, other tissues
Routes of administration of Non-Catecholamines
1) Oral drugs- GI tract absorption–> wide distribution
2) Inhaled drugs - gradual absorption from bronchi –> lower drug levels in the body
(e.g., Albuterol aka salbutamol for acute Asthma)
Adverse effects of Catecholamines
1) Palpitation
2) Tremors
3) Hypotension/ Hypertension
4) Stroke
5) Increased blood glucose levels
Name a few Direct-acting Catecholamine drugs
1) Epinephrine (Anaphylaxis &Asthma)
2) Norepinephrine ( Hypotension & Septic shock)
3) Dopamine (HF & unstable bradycardia)
4) Isoproterenol (Nebulizer acute asthma)
5) Dobutamine (HF)
Name a few direct-acting Non-Catecholamine drugs
1) Phenylephrine (nasal decongestant)
2) Clonidine & Methyldopa (mild/moderate Hypertension)
3) Isoproterenol (Bronchospasm, Heart block)
4) Dobutamine (CHF)
5) Albuterl -aka Salbutamol (Acute asthma/COPD)
6) Trebutaline (Premature labor)
Indication of Norepinepherine
1) Septic shock
2) Hypotension
MoA of Norepinepherine
NE effects : α1, α2, β1
–> α1- ↑ BP & ↑ TPR
–> β1- ↑HR, ↑SV, ↑CO, ↑ pulse pressure
–> potenital refelx bradychardia
NO EFFECT ON β2
Administration of Norepinephrine
IV admin only.
Adverse Effects of Norepinephrine
1) Vasospasm,
2) tissue necrosis,
3) excessive blood pressure increase,
4) arrhythmias,
5) cardiac infraction
Indication of Epinephrine
1) Anaphylaxis
2) Asthma
MoA of Epinephrine
1) Dose-dependent effects:
- Low-dose: β1, β2 stimulation
- High-dose: α1, β1 (β2).
2) β2-specific effects:
- Smooth muscle relaxation: bronchioles, uterus, blood vessels
3) Metabolic effects:
- ↑ glycogenolysis (muscle and liver).
- ↑ gluconeogenesis.
- ↑ mobilization and use of fat